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169445 [2018/11/20 14:26] (current)
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 +====== Histidine modification with diethyl pyrocarbonate shows heterogeneity of benzodiazepine receptors.======
 +
 +** Article date:** 1981/6/1
 +~~META:date created = 1981-06-01~~
 +
 +** PubMed ID: 169445 **
 +
 +** Journal name: Proceedings of the National Academy of Sciences of the United States of America (ISSN: 0027-8424) **
 +
 +** ABSTRACT **
 +
 +The effect of diethyl pyrocarbonate modification of histidine on the specific binding of [3H]diazepam and its enhancement with muscimol and (+/​-)-pentobarbital was investigated. Diethyl pyrocarbonate treatment produced a dose-related inhibition of specific [3H]diazepam binding to rat brain membranes with a maximal inhibition of approximately 40% at 1 mM. Scatchard analysis of the binding data showed that diethyl pyrocarbonate,​ while having no effect on the affinity (Kd), decreased the binding capacity (Bmax) of diazepam from a control value of 1543 +/- 116 fmol/mg of protein to 789 +/- 79 fmol/mg of protein (mean +/- SD; P less than 0.005; n = 4). Under conditions in which approximately 40% of the diazepam binding sites were modified by diethyl pyrocarbonate treatment, the ability of muscimol and pentobarbital to enhance diazepam binding was not altered. These results suggest that a histidine residue is critical for a part (approximately 40%) of the benzodiazepine binding sites and that there may exist a heterogeneity of benzodiazepine binding sites. Furthermore,​ these results indicate that perhaps only a portion of the benzodiazepine binding sites are functionally coupled to the gamma-aminobutyric acid receptor-ionophore complex.
 +
 +===== ===== 
 +
 +Author List: Burch T P, Ticku M K
 +
 +Publication Types: Journal Article; Research Support, U.S. Gov't, P.H.S.
 +
 +Substances mentioned in the article: Formates; Receptors, Drug; Receptors, GABA-A; Receptors, Neurotransmitter;​ Benzodiazepines;​ Muscimol; Histidine; Pentobarbital;​ Diethyl Pyrocarbonate;​ Diazepam; ​
 +
 +Mesh terms: Animals; Benzodiazepines/​metabolism;​ Brain; Chemical Phenomena; Chemistry; Diazepam/​metabolism;​ Diethyl Pyrocarbonate/​pharmacology;​ Formates/​pharmacology;​ Histidine; Male; Muscimol/​pharmacology;​ Pentobarbital/​pharmacology;​ Rats; Receptors, Drug/drug effects; Receptors, GABA-A; Receptors, Neurotransmitter/​drug effects; ​
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 +Citations: ​  - //​[[4155790]]//​
 +  - //​[[4240021]]//​
 +  - //​[[241459]]//​
 +  - //​[[4002]]//​
 +  - //​[[20632]]//​
 +  - //​[[918669]]//​
 +  - //​[[26577]]//​
 +  - //​[[207968]]//​
 +  - //​[[672418]]//​
 +  - //​[[27722]]//​
 +  - //​[[209854]]//​
 +  - //​[[763321]]//​
 +  - //​[[40257]]//​
 +  - //​[[6247012]]//​
 +  - //​[[6257534]]//​
 +  - //​[[6261261]]//​
 +  - //​[[7264652]]//​
 +  - //​[[14907713]]//​
 +  - //​[[13861983]]//​
 +  - //​[[209272]]//​
 +  - //​[[169445]]//​
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 +{{tag> Receptors,​_Neurotransmitter Diethyl_Pyrocarbonate Pentobarbital Receptors,​_GABA-A Diazepam Receptors,​_Drug Histidine Benzodiazepines Muscimol Formates }}
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 +{{keywords>​ Receptors, Neurotransmitter,​ Diethyl Pyrocarbonate,​ Pentobarbital,​ Receptors, GABA-A, Diazepam, Receptors, Drug, Histidine, Benzodiazepines,​ Muscimol, Formates}}
 +
  
169445.txt ยท Last modified: 2018/11/20 14:26 (external edit)